规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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Other Sizes |
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药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
Dermal penetration of (14)C-labeled abate was measured in rats, rabbits, and dogs. Absorption was assessed by monitoring excreted radioactivity in urine and feces for 7 days and analysis of tissue specimens /were conducted/. Absorption would be expected to be less than 3% of applied dose. No evidence of bodily retention or pooling of radioactive moiety was demonstrated. In guinea pig, /oral/ absorption apparently was less than in rat, & biliary excretion of metabolites was demonstrated. When (3)H temephos was administered to rats by mouth, radioactivity reached a peak in the blood between 5 and 8 hr and then dissipated within a half-life of about 10 hr. Appreciable radioactivity was found only in the GI tract and fat. Both in the feces and in the fat, most of the radioactivity came from unchanged insecticide, but small amounts of the sulfoxide were present also. Traces of temephos were found in the urine ... . In mammals, elimination of mainly of unchanged temephos in the feces and urine. Metabolism / Metabolites Studies with tritium-labeled abate indicated that this insecticide was relatively resistant to metabolic degradation. Residues on bean leaves ... consisted primarily of intact abate- about 70% of applied dose. The major metabolite was the sulfoxide derivative- less than 5% of the dose. Traces of sulfone derivative, oxygen analog, and glucosidic conjugates of phenolic hydrolysis products from abate and its sulfoxide & sulfone derivatives were also observed. When rats were fed Abate, 60% of the material appeared in ... feces as the oxygen analog of Abate and its sulfoxide. The thiodiphenol, sulfinyldiphenol and sulfonyldiphenol were also found. In the urine, sulfate and glucoside conjugates of the hydrolysis products of Abate and sulfoxide as well as sulfone analogs accounted for 39.5% of the material administered. ... Five compounds found in feces and three in urine were not identified. Larvae of the mosquito (Aedes aegypti L) metabolized Abate to sulfoxides and sulfones of Abate, the oxygen analog, and the demethylated analog. Some conjugates were also formed. In the housefuly, all expected metabolic products were found internally either as the intact ester or as hydrolyzed material ... Abate yields in rat, abate sulfoxide and thiodiphenol. /From table/ For more Metabolism/Metabolites (Complete) data for TEMEPHOS (8 total), please visit the HSDB record page. Biological Half-Life When (3)H temephos was administered to rats by mouth, radioactivity reached a peak in blood between 5 & 8 hr & then dissipated with half-life of about 10 hr. |
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毒性/毒理 (Toxicokinetics/TK) |
Interactions
Mixture of abate and malathion are appreciably more toxic in rats than either compound alone. Non-Human Toxicity Values LD50 Rabbit female dermal 970 mg/kg LD50 Rabbit male dermal 1930 mg/kg LD50 Rat oral male 8600 mg/kg LD50 Rat oral female 13,000 mg/kg For more Non-Human Toxicity Values (Complete) data for TEMEPHOS (15 total), please visit the HSDB record page. |
其他信息 |
Temephos appears as white crystalline solid or liquid (above 87 °F). Used as an insecticide. Technical grade is a viscous brown liquid. (NIOSH, 2024)
Temephos is an organic sulfide that is diphenyl sulfide in which the hydrogen at the para position of each of the phenyl groups has been replaced by a (dimethoxyphosphorothioyl)oxy group. It has a role as an EC 3.1.1.7 (acetylcholinesterase) inhibitor, an acaricide, an agrochemical and an ectoparasiticide. It is an organic thiophosphate, an organothiophosphate insecticide and an organic sulfide. It is functionally related to a 4,4'-thiodiphenol. Diphos has been used in trials studying the treatment of Plasmodium Falciparum Malaria. An organothiophosphate insecticide. Mechanism of Action Abate is a cholinesterase inhibiting insecticide. Organophosphates poison insects and humans primarily by phosphorylation of the acetylcholinesterase enzyme at nerve endings. /Organophosphate Cholinesterase-inhibiting pesticides/ |
分子式 |
C16H20O6P2S3
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分子量 |
466.46
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精确质量 |
465.989
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CAS号 |
3383-96-8
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相关CAS号 |
Temephos-d12;1219795-39-7
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PubChem CID |
5392
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外观&性状 |
Colorless crystals
White, crystalline solid or liquid (above 87 degrees F) [Note: Technical grade is a brown, viscous liquid]. |
密度 |
1.4±0.1 g/cm3
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沸点 |
518.5±60.0 °C at 760 mmHg
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熔点 |
30-31°C
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闪点 |
267.4±32.9 °C
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蒸汽压 |
0.0±1.3 mmHg at 25°C
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折射率 |
1.613
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LogP |
5.96
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tPSA |
164.48
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氢键供体(HBD)数目 |
0
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氢键受体(HBA)数目 |
9
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可旋转键数目(RBC) |
10
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重原子数目 |
27
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分子复杂度/Complexity |
474
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定义原子立体中心数目 |
0
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SMILES |
COP(OC(C=C1)=CC=C1SC2=CC=C(OP(OC)(OC)=S)C=C2)(OC)=S
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InChi Key |
WWJZWCUNLNYYAU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C16H20O6P2S3/c1-17-23(25,18-2)21-13-5-9-15(10-6-13)27-16-11-7-14(8-12-16)22-24(26,19-3)20-4/h5-12H,1-4H3
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化学名 |
[4-(4-dimethoxyphosphinothioyloxyphenyl)sulfanylphenoxy]-dimethoxy-sulfanylidene-λ5-phosphane
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别名 |
Bithion; Abate; Temefos
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
DMSO : ~100 mg/mL (~214.38 mM)
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溶解度 (体内实验) |
配方 1 中的溶解度: 2.5 mg/mL (5.36 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 悬浮液;超声助溶。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (5.36 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1438 mL | 10.7190 mL | 21.4381 mL | |
5 mM | 0.4288 mL | 2.1438 mL | 4.2876 mL | |
10 mM | 0.2144 mL | 1.0719 mL | 2.1438 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。